Anticancer Activity of Artemisinin and its Derivatives

Anticancer Res. 2017 Nov;37(11):5995-6003. doi: 10.21873/anticanres.12046.


Artemisinin is an extract from the plant Artemisia annua. With its semi-synthetic derivatives, they form a group of well-known and efficacious antimalarial drugs. Recent studies have documented the potential anticancer effect of artemisinin and its derivatives (ARTs). This review summarizes results of preclinical studies, documenting mechanisms of anticancer actions of ARTs and clinical studies focused mainly on efficacy, safety and dose-ranging of ARTs as anticancer chemotherapeutics. The main mechanisms of action of ARTs is the production of reactive oxygen species, inhibition of cell cycle in G0/G1 phase, induction of apoptosis and inhibition of angiogenesis. Safety studies have shown no evident toxicity and low incidence of adverse effects. ARTs potential to inhibit growth of solid tumours suggests their application in a neoadjuvant therapy. Dihydroartemisinin and artesunate exhibit chemosensitising effects in vivo in breast, lung, pancreas and glioma cancer cells, proposing the use of ARTs also in combination anticancer therapy.

Keywords: Artemisinin; Artesunate; anticancer activity; dihydroartemisinin; review.

Publication types

  • Review

MeSH terms

  • Animals
  • Antimalarials / pharmacology*
  • Antineoplastic Agents / pharmacology*
  • Artemisinins / chemistry*
  • Artemisinins / pharmacology*
  • Humans
  • Neoplasms / drug therapy*


  • Antimalarials
  • Antineoplastic Agents
  • Artemisinins